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117175

Radioiodination of 5-aminoisoquinoline for Poly (ADP-ribose) Polymerase Targeting: An In vitro Evaluation in Colorectal Carcinoma Cells

Article

Last updated: 22 Jan 2023

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Abstract

THE ISOQUINOLINE derivative, 5-aminoisoquinoline (5-AIQ), is a potent inhibitor of poly (ADP-ribose) polymerase (PARP) activity; the DNA repairing protein frequently overexpressed in various carcinoma cells. The current study is dedicated for developing a highly specific radioiodinated PARP-1 binding tracer namlely, [131I] 5-aminoisoquinoline. The radioiodination of 5-aminoisoquinoline with 131I was carried out via electrophilic substitution reaction. In order to achieve the maximum radioiodination, the parameters including 5-aminoisoquinoline concentration, oxidizing agent, reaction time, temperature and type of solvent were optimized. the radiochemical purity was determined by high performance liquid chromatography (HPLC) using Reversed phase lichrosorb column 250×4.6 mm, C-18 5 μm. The maximum radiochemical yield was 80% with radiochemical purity reached 98%. The log P value for [131I] 5-aminoisoquinoline was found to be 2.08 ± 0.79. Data presented from Cell viability (MTT) cytotoxicity assay on Caco-2 cells showed matched IC50 values with the selected drug concentrations profile for either labeled or unlabeled 5-aminoisoquinoline. Likewise, the radioiodinated 5-aminoisoquinoline elucidated a higher cell uptake compared to free I-131.

DOI

10.21608/ejrsa.2020.36220.1101

Keywords

5-aminoisoquoline, Colorectal adenocarcinoma (Caco-2) cell line, PARP, Radiolabeling

Authors

First Name

Tarek

Last Name

EL-Hamoly

MiddleName

-

Affiliation

Cyclotron Project, Nuclear Research Center, Atomic Energy Authority, Egypt , Drug Radiation Research Department, National Center for Radiation Research and Technology, Atomic Energy Authority, Egypt

Email

tahamoly@hotmail.com

City

-

Orcid

0000-0001-5246-2168

First Name

Hany

Last Name

Aglan

MiddleName

-

Affiliation

Cyclotron Project, Egyptian Atomic Energy Authority Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, Egypt

Email

hany3glan2@yahoo.com

City

-

Orcid

-

First Name

Mogahed

Last Name

Alabyad

MiddleName

-

Affiliation

Cyclotron Project, Nuclear Research Center, Atomic Energy Authority, Egypt

Email

alabyad_m@yahoo.com

City

-

Orcid

-

First Name

Shaban

Last Name

Kandil

MiddleName

-

Affiliation

Cyclotron Project, Nuclear Research Center, Atomic Energy Authority, Egypt , Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, Egypt

Email

shaban_kandil@yahoo.com

City

-

Orcid

-

Volume

33

Article Issue

1

Related Issue

17957

Issue Date

2020-07-01

Receive Date

2020-07-25

Publish Date

2020-07-01

Page Start

59

Page End

64

Print ISSN

1110-0303

Online ISSN

2314-8527

Link

https://ejrsa.journals.ekb.eg/article_117175.html

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https://ejrsa.journals.ekb.eg/service?article_code=117175

Order

8

Type

Original Article

Type Code

136

Publication Type

Journal

Publication Title

Egyptian Journal of Radiation Sciences and Applications

Publication Link

https://ejrsa.journals.ekb.eg/

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Article

Created At

22 Jan 2023